4,4A-Dihydroxanthones as Promising Compounds for Creation of New Antimicrobials

Autor: V. V. Frolova, S. V. Gurina, N. M. Chernov, I. P. Yakovlev
Jazyk: ruština
Rok vydání: 2020
Předmět:
Zdroj: Антибиотики и Химиотерапия, Vol 64, Iss 11-12, Pp 3-7 (2020)
Druh dokumentu: article
ISSN: 0235-2990
DOI: 10.1016/0235-2990-2019-64-11-12-3-7
Popis: In order to predict the biological activity of the new derivatives of 4,4a-dihydroxanthone, the PASS (Prediction ofActivity Spectra for Substances) computer program was used. It allows predicting the biological activity spectrum of chemical compounds based on the analysis of structure-activity interrelation. Derivatives of 4,4a-dihydroxanthone were synthesized at the Department of Organic Chemistry of the Saint Petersburg State Chemical Pharmaceutical University. As a result of the screening, it was found that 4,4a-dihydroxanthones can exhibit antibacterial, antifungal, antitumor, and antiviral effects. Antimicrobial activity of the obtained compounds was studied against Gram-positive and Gram-negative bacteria, as well as fungi. Dihydroxanthones were shown to have an inhibitory effect on Gram-positive bacteria. Relationship between the structure of derivatives and their antimicrobial activity is established. The presence of electron-withdrawing substituents led to an increase in activity, and electron-donating substituents reduced the antibacterial effect of the compounds. The most active compound, 5-bromo-7-chloro-4,4a-dihydrox-anthone, was found to be active against certain clinical strains of staphylococci.
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